摘要
以5-溴-2-氯苯甲酸为原料,经酰氯化、傅克酰化反应、还原得中间体5-溴-2-氯-4'-乙氧基二苯甲烷,该中间体与2,3,4,6-四-O-三甲基硅基-D-葡萄糖酸内酯经缩合、醚化、脱甲氧基、酯化、脱保护得目标化合物,总收率45%,纯度99.1%,其结构经1H NMR及MS确证。
Dapagliflozin was synthesized from 5-bromo-2-chlorobenzoic acid via chlorination,Friedel-Crafts acylation reaction and reduction to give 5-bromo-2-chloro-4＇-ethoxyldiphenylmethane,which was condensed with 2,3,4,6-tetra-O-trimethylsilyl-D-glucono-1,5-lactone.Finally,dapagliflozin was obtained wia the removal of the methoxy,esterification and deprotection with an overall yield of 45% and a purity of 99. 1%. The target compound was characterized by1 H NMR and MS.
出处
《化学研究与应用》
CAS
CSCD
北大核心
2016年第4期530-533,共4页
Chemical Research and Application
